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Biological Activity

Protocol

Technical Information

Purity & Documentation

References

Description

EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.
In vitro: EPZ031686 have a cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibition. The first SMYD3 inhibitor identify to show double-digit nanomolar cellular activity. EPZ031686 show < 30% inhibition against 16 histone methyltransferase targets at a 10 uM screening concentration.
In vivo: EPZ031686 show good bioavailability following oral dosing in mice. The administration for mice is 1 mg/kg by i.v.